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4,778 results
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Spiropiperidines as high-affinity, selective sigma ligands.
Chambers MS, Baker R, Billington DC, Knight AK, Middlemiss DN, Wong EH. Chambers MS, et al. J Med Chem. 1992 May 29;35(11):2033-9. doi: 10.1021/jm00089a013. J Med Chem. 1992. PMID: 1317923
N-Arylsulfonylindole derivatives as serotonin 5-HT(6) receptor ligands.
Russell MG, Baker RJ, Barden L, Beer MS, Bristow L, Broughton HB, Knowles M, McAllister G, Patel S, Castro JL. Russell MG, et al. J Med Chem. 2001 Nov 8;44(23):3881-95. doi: 10.1021/jm010943m. J Med Chem. 2001. PMID: 11689074
Controlled modification of acidity in cholecystokinin B receptor antagonists: N-(1,4-benzodiazepin-3-yl)-N'-[3-(tetrazol-5-ylamino) phenyl]ureas.
Castro JL, Ball RG, Broughton HB, Russell MG, Rathbone D, Watt AP, Baker R, Chapman KL, Fletcher AE, Patel S, Smith AJ, Marshall GR, Ryecroft W, Matassa VG. Castro JL, et al. J Med Chem. 1996 Feb 16;39(4):842-9. doi: 10.1021/jm9506736. J Med Chem. 1996. PMID: 8632408
Synthesis and characterization of all four isomers of the muscarinic agonist 2'-methylspiro[1-azabicyclo[2.2.2]octane-3,4'-[1,3]dioxolane].
Saunders J, Showell GA, Baker R, Freedman SB, Hill D, McKnight A, Newberry N, Salamone JD, Hirshfield J, Springer JP. Saunders J, et al. J Med Chem. 1987 Jun;30(6):969-75. doi: 10.1021/jm00389a003. J Med Chem. 1987. PMID: 3585909
Detailed biological evaluation of each isomer indicated that while the 3(R),2'(S) isomer was the most active in binding studies, it was the 3(R),2'(R) isomer that displayed the largest functional selectivity between ganglion (M-1 site) and heart (M-2 site). . …
Detailed biological evaluation of each isomer indicated that while the 3(R),2'(S) isomer was the most active in binding studies, it w …
Novel benzodiazepine receptor partial agonists: oxadiazolylimidazobenzodiazepines.
Watjen F, Baker R, Engelstoff M, Herbert R, MacLeod A, Knight A, Merchant K, Moseley J, Saunders J, Swain CJ, et al. Watjen F, et al. J Med Chem. 1989 Oct;32(10):2282-91. doi: 10.1021/jm00130a010. J Med Chem. 1989. PMID: 2552115
2-Methyl-1,3-dioxaazaspiro[4.5]decanes as novel muscarinic cholinergic agonists.
Saunders J, Showell GA, Snow RJ, Baker R, Harley EA, Freedman SB. Saunders J, et al. J Med Chem. 1988 Feb;31(2):486-91. doi: 10.1021/jm00397a039. J Med Chem. 1988. PMID: 3339620
Tachykinin NK1 receptor antagonists act centrally to inhibit emesis induced by the chemotherapeutic agent cisplatin in ferrets.
Tattersall FD, Rycroft W, Francis B, Pearce D, Merchant K, MacLeod AM, Ladduwahetty T, Keown L, Swain C, Baker R, Cascieri M, Ber E, Metzger J, MacIntyre DE, Hill RG, Hargreaves RJ. Tattersall FD, et al. Neuropharmacology. 1996;35(8):1121-9. doi: 10.1016/s0028-3908(96)00020-2. Neuropharmacology. 1996. PMID: 9121615
Synthesis and biological activity of 3-[2-(dimethylamino)ethyl]-5-[(1,1-dioxo-5-methyl-1,2,5-thiadiazolidin- 2-yl)-methyl]-1H-indole and analogues: agonists for the 5-HT1D receptor.
Castro JL, Baker R, Guiblin AR, Hobbs SC, Jenkins MR, Russell MG, Beer MS, Stanton JA, Scholey K, Hargreaves RJ, et al. Castro JL, et al. J Med Chem. 1994 Sep 16;37(19):3023-32. doi: 10.1021/jm00045a006. J Med Chem. 1994. PMID: 7932524
Effect of plasma protein binding on in vivo activity and brain penetration of glycine/NMDA receptor antagonists.
Rowley M, Kulagowski JJ, Watt AP, Rathbone D, Stevenson GI, Carling RW, Baker R, Marshall GR, Kemp JA, Foster AC, Grimwood S, Hargreaves R, Hurley C, Saywell KL, Tricklebank MD, Leeson PD. Rowley M, et al. J Med Chem. 1997 Dec 5;40(25):4053-68. doi: 10.1021/jm970417o. J Med Chem. 1997. PMID: 9406596
These measures of plasma protein binding correlate well (r = 0.84), and the HPLC assay has been used extensively to quantify plasma protein binding. For the 4-hydroxyquinolone series, binding to plasma protein correlates (r = 0.92) with log P (octanol/pH 7.4 buffer) …
These measures of plasma protein binding correlate well (r = 0.84), and the HPLC assay has been used extensively to quantify plasma p …
4-Heterocyclylpiperidines as selective high-affinity ligands at the human dopamine D4 receptor.
Rowley M, Collins I, Broughton HB, Davey WB, Baker R, Emms F, Marwood R, Patel S, Patel S, Ragan CI, Freedman SB, Ball R, Leeson PD. Rowley M, et al. J Med Chem. 1997 Jul 18;40(15):2374-85. doi: 10.1021/jm970111h. J Med Chem. 1997. PMID: 9240352
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